مرکز منطقه ای اطلاع رساني علوم و فناوري - Benzodiazepine receptors mediated anxiolytic-like effects of some 1,3,5-triaryl-4,5-dihydro-1h-pyrazole derivatives

Author/Authors :

Can, Özgür Devrim Anadolu Üniversitesi - Eczacılık Fakültesi - Farmakoloji Anabilim Dalı, Turkey , Turan, Nazlı Anadolu Üniversitesi - Eczacılık Fakültesi - Farmakoloji Anabilim Dalı, Turkey , Alyu, Feyza Anadolu Üniversitesi - Eczacılık Fakültesi - Farmakoloji Anabilim Dalı, Turkey

Abstract :

Purpose: Pyrazole is a heterocycle structure characterized by a five-membered ring of three carbon and two adjacent nitrogen atoms. Numerous compounds including pyrazole nucleus have been reported to possess wide diverse of pharmacological activities related to central nervous system. Based on this knowledge, in the present study, we planned to examine probable anxiolytic-like effects of eighteen 1,5-diaryl-3-[4-(methylsulfonyl)phenyl]-4,5-dihydro-1H-pyrazole derivative test compounds (2a-s) which previously synthesized by our research group. Material and Methods: Anxiolytic activity potential of the test compounds (100 mg/kg, i.p) was evaluated in mice using hole-board and plus-maze tests. An antagonism study was conducted with flumazenil (3 mg / kg, ip), a GABA-benzodiazepine receptor blocker, in order to investigate mechanism of the anxiolytic-like activities. Results: In the hole-board tests, compounds 2g, 2h, 2k and 2s significantly increased total number of the head-dipping behavior and number of the explored holes. In the plus-maze tests, the same compounds increased the time spent in the open arms and the number of entries into the open arms. These findings indicated that these four compounds have anxiolytic-like effects. Reference drug diazepam (1 mg/kg, i.p) also showed its anxiolytic activity in both of the tests, as expected. Conclusion: Benzodiazepine receptors mediated the anxiolytic-like effects of 2g, 2h, 2k and 2s coded 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivative compounds.